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. Author manuscript; available in PMC: 2016 Feb 12.
Published in final edited form as: J Med Chem. 2015 Jan 23;58(3):1307–1319. doi: 10.1021/jm5015742

Table 4.

In vitro ADME data for compounds 2 and 19.

Compound mean A->B Papp (×10-6cm s-1) Test species Mean remaining parent, with NADPH (%) Mean remaining parent, free of NADPH (%)
2 18.7 Human 96.8 84.8
Mouse 79.4 110
19 16.5 Human 90.7 106
Mouse 77.6 102
Verapamile Human 8.4 89.4
Mouse 6.0 96.5
Warfarin 25.3 Human 102 96.7
Mouse 104 101
Ranitidine 0.24

Papp: Caco 2 apparent permeability. Permeability ranking: Low: <0.5; Moderate: 0.5 - 5; High: > 5. For permeability measurements 10 μM concentration was used and 2 h assay time. For metabolic stability, 1 μM concentration and 0 and 60 min incubation time was used. Test species represent either human or mouse microsomes.